Benzenesulfon YL-semicarbazides for lowering blood sugar levels

Abstract

Hypoglycemically active benzenesulfonyl-semicarbazides of the formula ##SPC1## Wherein X is hydrogen, chlorine, bromine, methyl or methoxy, Y is --CH(CH 3 )-CH 2 --, preferably --CH 2 --CH 2 --, Z is hydrogen or a hydrocarbon radical of 1 or 2 carbon atoms, which forms together with Y a 5- or 6-membered ring, R is alkylene-imino of 3 to 7 carbon atoms in the ring which may be unsaturated or substituted by 1 or 2 methyl or lower alkyl or methoxy, pentamethylene-imino substituted by endoalkylene of 1 to 3 carbon atoms, hexamethylene-imino substituted by endoethylene in β- ε-position, tetrahydro-iso-indoline, 4,7-endoalkylenehexahydro- or -tetrahydro-iso-indoline, the endoalkylene containing 1 or 2 carbon atoms and the double bond of the tetrahydro compound being in 5,6-position, and the salts thereof as pharmaceutical preparations for oral administration and lowering of blood sugar level in the treatment of diabetes mellitus and the process for lowering the blood sugar level in the treatment of diabetes mellitus.

We claim: 
     
       1. A pharmaceutical preparation for oral administration and lowering the blood sugar level in the treatment of diabetes mellitus, which comprise a pharmaceutical carrier and about 0.5 to 100 mg. per unit dose of a benzenesulfonyl-semicarbazide of the formula ##SPC10## in which   X represents hydrogen, chlorine, bromine, methoxy or methyl,   Z is hydrogen or alkylene of 1 or 2 carbon atoms, which forms together with Y a 5-membered ring,   Y represents --CH(CH 3 )--CH 2  --, or --CH 2  --CH 2  --,   R represents a. alkylene-imino of 3 to 7 carbon atoms in the ring, which may be unsaturated or substituted by 1 or 2 methyl groups or lower alkyl group or methoxy group, a salt thereof of a pharmaceutically acceptable base or acid.       
     
     
       2. A pharmaceutical preparation for oral administration and lowering the blood sugar level in the treatment of diabetes mellitus according to claim 1 wherein the semicarbazide is 4-[4-(β-6-chloro-quinolino-8-carboxamido-ethyl)-benzenesulfonyl]-1,1-(3-methyl-pentamethylene)semicarbazide. 
     
     
       3. A process for lowering the blood sugar level in the treatment of diabetes mellitus, which comprises administering orally to the patient an effective amount in a unit dose from about 0.5 to 100 mg. of a benzenesulfonyl-semicarbazide as defined in claim 1 or a salt thereof of a pharmaceutically acceptable base or acid.